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Compound Detail

CHEMBL1783244

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CCCN1Cc2nc3c(CC(C)(C)C)cccc3c(N)c2C1=O

Basic Information

ChEMBL ID CHEMBL1783244
Phase Preclinical
Structure Type MOL
InChI Key JEUGTSHICBOMGA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

311.4
MW (Da)
3.77
ALogP
3
HBA
1
HBD
59.2
PSA (Ų)
0.94
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H25N3O
MW 311.43
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.56

Activity Summary

Ki 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-2/beta-3/gamma-2
CHEMBL2094130
Ki 8.0 8.0 10.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 230.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21498079 10.1016/j.bmc.2011.03.035 GABA-A receptor; alpha-2/beta-3/gamma-2 2
21498079 10.1016/j.bmc.2011.03.035 No relevant target 1
21498079 10.1016/j.bmc.2011.03.035 Liver microsomes 1
21498079 10.1016/j.bmc.2011.03.035 GABA-A receptor; alpha-1/beta-2/gamma-2 1

Data from ChEMBL 36 via Core Engine